Article
A Phenotypic Screen for Small-Molecule Inhibitors of Constitutively Active Mutant Thrombopoietin Receptor Implicated in Myeloproliferative Neoplasms.
Combinatorial chemistry & high throughput screening - 1 Jan 2016
Ngo Anna, Koay Ann Zhufang, Pecquet Christian, Diaconu Carmen C, Ould-Amer Yasmine, Huang Qiwei, Kang Congbao, Poulsen Anders, Lee May Ann, Jenkins David, Shiau Andrew, Constantinescu Stefan N, Choong Meng Ling
Abstract excerpt
BACKGROUND: Rather than a Janus Kinase 2 inhibitor (ruxolitinib), a specific thrombopoietin receptor (TpoR) inhibitor would be more specific for the treatment of myeloproliferative neoplasms due to TpoR mutations. OBJECTIVE: A cell-based phenotypic approach to identify specific TpoR inhibitors was implemented and a library of 505,483 small molecules was screened for inhibitory effects on cells transformed by TpoR...
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